Atef M, Youssef S A, Atta A H, el-Maaz A A
Department of Pharmacology, Faculty of Veterinary Medicine, Cairo University, Giza, Egypt.
Dtsch Tierarztl Wochenschr. 1991 Dec;98(12):451-3.
The disposition kinetics of tylosin was studied in goats after intravenous or intramuscular injection of 15 mg/kg b. wt. Following i.v. injection, tylosin was rapidly and widely distributed in goats (half life of distribution: 0.2 h and volume of distribution: 1.7 l/kg). It was slowly eliminated with a mean elimination half life of 3.04 h and a total body clearance rate of 6.8 ml/kg/min. Following i.m. injection, tylosin was slowly absorbed (T1/2ab of 1.82 h). Tylosin concentration in serum was greater than 1 microgram/ml after 1 h and persisted up to 12 h post-injection. The peak concentration (Cmax, 2.38 micrograms/ml) was obtained after 4.19 h. The systemic bioavailability of tylosin injected intramuscularly was 72.6% and the serum protein bound fraction was 37.6% of the total drug. Tylosin was excreted in milk and urine at concentrations much higher than that in serum. Low concentrations of tylosin were reported in ruminal juice of goats. In conclusion tylosin should be injected every 15 hours to obtain an appreciable concentration in serum, milk and urine.
在山羊静脉注射或肌肉注射15mg/kg体重的泰乐菌素后,对其处置动力学进行了研究。静脉注射后,泰乐菌素在山羊体内迅速广泛分布(分布半衰期:0.2小时,分布容积:1.7l/kg)。它消除缓慢,平均消除半衰期为3.04小时,全身清除率为6.8ml/kg/分钟。肌肉注射后,泰乐菌素吸收缓慢(吸收半衰期为1.82小时)。注射1小时后血清中泰乐菌素浓度大于1微克/毫升,并在注射后持续12小时。4.19小时后达到峰值浓度(Cmax,2.38微克/毫升)。肌肉注射泰乐菌素的全身生物利用度为72.6%,血清蛋白结合率占总药物的37.6%。泰乐菌素在牛奶和尿液中的排泄浓度远高于血清中的浓度。据报道,山羊瘤胃液中泰乐菌素浓度较低。总之,应每15小时注射一次泰乐菌素,以便在血清、牛奶和尿液中获得可观的浓度。